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    PURINONE COMPOUNDS AS KINASE INHIBITORS
    41.
    发明专利
    PURINONE COMPOUNDS AS KINASE INHIBITORS 未知

    公开(公告)号：CA2917167A1

    公开(公告)日：2015-01-08

    申请号：CA2917167

    申请日：2014-06-30

    Applicant: PHARMACYCLICS LLC

    Inventor： CHEN WEI ,  JIA ZHAOZHONG J ,  LOURY DAVID J

    IPC: C07D473/34 ,  A61K31/52 ,  A61P19/02 ,  A61P37/00

    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

    Inhibitors of Bruton's tyrosine kinase
    43.
    发明专利
    Inhibitors of Bruton's tyrosine kinase 未知

    公开(公告)号：AU2013276959A1

    公开(公告)日：2014-01-16

    申请号：AU2013276959

    申请日：2013-12-19

    Applicant: PHARMACYCLICS LLC

    Inventor： HONIGBERG LEE ,  VERNER ERIK ,  BUGGY JOSEPH J ,  LOURY DAVID ,  CHEN WEI

    IPC: C07D253/06 ,  A61K31/519 ,  A61K31/52 ,  A61P29/00 ,  A61P35/00 ,  C07D473/34 ,  C07D487/04

    Abstract: INHIBITORS OF BRUTON'S TYROSINE KINASE 1005171 Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further 5 described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. S Cmpd Cell line Gl5 (uM) WSU-NHL 0.12 Mino 0.15 WSU-DLCL2 0.5 Ramos 5.5 HF1 >10 LY19 >10 LY3 >10 :DB >10 DLCL2 Xenograft -o-vehicle 400 -- ~Cmpd 1 10mg/kg -U- Cmpd 1 30mg/kg 300 --+- Cmpd 1 90mg/kg 2 300 -.... - - -.... . ..... 0 3 6 9 12 15 18 Day DOHH2 Xenograft -c-vehicle 700 --- m- Cmpd 1 25mg/kg BID 500 ........ .......... E 300 - - - -- - 100 or 0 5 Day 10 15 Figure 1

    INHIBIDORES DE TIROSINA CINASA DE BRUTON
    46.
    发明专利
    INHIBIDORES DE TIROSINA CINASA DE BRUTON 未知

    公开(公告)号：DOP2016000071A

    公开(公告)日：2016-09-15

    申请号：DO2016000071

    申请日：2016-03-29

    Applicant: PHARMACYCLICS LLC

    Inventor： CHEN WEI ,  LOURY DAVID J ,  WANG LONGCHENG ,  JIA ZHAOZAHONG J

    IPC: A61K31/519 ,  A61P19/00 ,  A61P19/02 ,  C07D401/14 ,  C07D403/14

    Abstract: EN LA PRESENTE SE DESCRIBEN COMPUESTOS QUE FORMAN ENLACES COVALENTES CON LA TIROSINA CINASA DE BRUTON (BTK). TAMBIÉN SE DESCRIBEN INHIBIDORES IRREVERSIBLES DE BTK. ADEMÁS, TAMBIÉN SE DESCRIBEN LOS INHIBIDORES REVERSIBES DE BTK. TAMBIÉN SE DESCRIBEN COMPOSICIONES FARMACÉUTICAS QUE INCLUYEN LOS COMPUESTOS. SE DESCRIBEN MÉTODOS PARA USAR INHIBIDORES DE BTK, SOLOS O EN COMBINACIÓN CON OTROS AGENTES TERAPÉUTICOS, PARA EL TRATAMIENTO DE ENFERMEDADES AFECCIONES AUTOINMUNITARIAS, ENFERMEDADES AFECCIONES HETEROINMUNITARIAS, CÁNCER, INCLUSIVE LINFOMA Y ENFERMEDADES AFECCIONES INFLAMATORIAS.

    DERIVADOS DE PIRAZOLO[3,4-d]PIRIMIDIN COMO INHIBIDORES IRREVERSIBLES DE LA TIROSINA CINASA DE BRUTON (BTK)
    47.
    发明专利
    DERIVADOS DE PIRAZOLO[3,4-d]PIRIMIDIN COMO INHIBIDORES IRREVERSIBLES DE LA TIROSINA CINASA DE BRUTON (BTK) 未知

    公开(公告)号：PE05602016A1

    公开(公告)日：2016-06-09

    申请号：PE0004272016

    申请日：2014-09-29

    Applicant: PHARMACYCLICS LLC

    Inventor： CHEN WEI ,  WANG LONGCHENG ,  LOURY DAVID J ,  JIA ZHAOZHONG J

    IPC: A61K31/519 ,  A61P19/00 ,  A61P19/02 ,  C07D401/14 ,  C07D403/14

    CPC classification number: C07D487/04

    Abstract: La presente invencion se refiere a derivados de pirazolo[3,4-d]pirimidin de formula (I), en donde: L1 es –N(R2)C(O)- o –C(O)N(R2)-; R1 es arilo C6-C12, entre otros; R2 es H o alquilo C1-C4; R4 es H, alquilo C1-C6, entre otros; R5 es cicloalquilo C3-C8, entre otros; R10 es halogeno, entre otros; m es 1 o 2; n es 0 o 1 y p es 0, 1 o 2. Son compuestos preferidos: (R,E)-4-(4-amino-1-(1-(4-(ciclopropil(metil)amino)but-2-enoil)pirrolidin-3-il)- 1H-pirazolo[3,4-d]pirimidin-3-il)-N-(4-metilpiridin-2-il)benzamida; (R,E)-4-(4-amino-1-(1-(4-(ciclopropil(metil)amino)but-2-enoil)pirrolidin-3-il)- 1H-pirazolo[3,4-d]pirimidin-3-il)-N-(4-(trifluorometil)piridin-2-il)benzamida, entre otros. Estos derivados actuan como inhibidores irreversibles de la Tirosina Cinasa de Bruton (Btk) siendo utiles en el tratamiento de enfermedades autoinmunitarias, heteroinmunitarias, cancer, inclusive linfoma y enfermedades inflamatorias

    Purinone compounds as kinase inhibitors
    49.
    发明专利
    Purinone compounds as kinase inhibitors 未知

    公开(公告)号：AU2013215166B2

    公开(公告)日：2016-04-21

    申请号：AU2013215166

    申请日：2013-01-30

    Applicant: PHARMACYCLICS LLC

    Inventor： CHEN WEI ,  LOURY DAVID J ,  YAN SHUNQI ,  WANG LONGCHENG ,  FRYE LEAH LYNN

    IPC: C07D473/32 ,  A61K31/52 ,  A61P35/00 ,  A61P37/00

    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

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